Oral delivery has long been regarded as the most preferred route of drug administration and over the years, research in this field has made significant strides despite the numerous challenges. Barriers limiting effective oral drug delivery include poor solubility, membrane permeability, hydrolysis or enzymatic degradation in the gastrointestinal (GI) tract, pre-systemic metabolism, and excretion of the active, among others. Drug developers and formulators, however, now recognize that better dosage form design can be achieved with proper characterization of the API’s physicochemical properties and an assessment of the potential formulation and manufacturing challenges during an early stage. Advances in oral drug delivery continue to open up new avenues for more patient-centric drug design that offer improved outcomes.